【作者】 宋沛然；

【导师】 陈百泉；

【作者基本信息】 河南大学 ， 中药学， 2008， 硕士

【摘要】 穿心莲超分子提取物(supramolecular extract from Andrographis paniculata(Burm.f.) Nees. SEA)系河南大学天然药物研究所新近开发的中药提取物,所用原料是爵床科植物穿心莲(Andrographis Paniculata(Burm.f.)Nees.)地上部分。穿心莲属清热药,有清热解毒,凉血消肿的功效,辩证用于“里热证”的治疗,《泉州本草》记:“清热解毒,消炎退肿。治咽喉炎症,痢疾,高热”。药理研究表明,穿心莲制剂在解热、抗炎、抗菌、抗病毒方面药效作用较强,临床广泛应用于感冒发热,急慢性咽炎,痢疾,内毒素血症等。目的:本研究对穿心莲超分子提取物进行急性毒性和主要药效学研究,为临床安全合理用药提供药理实验依据。在药效学研究基础上,对SEA的抗炎机制进行探讨。方法:研究内容分三个部分:一. SEA的急性毒性研究腹腔注射给药的急性毒性试验求得SEA的半数致死量(LD50)为717.8mg·kg-1。二.SEA的主要药效学研究1.解热试验SEA的高剂量(600mg·kg-1),中剂量(300mg·kg-1)连续三天给药可显著降低干酵母所致大鼠发热反应和二硝基苯酚所致大鼠发热反应,与空白对照组比较有明显的差异(P<0.01和P<0.05),与等剂量的穿心莲内酯组无显著性差异。2.抗炎试验SEA的高剂量(600mg·kg-1),中剂量(300mg·kg-1)连续三天给药可显著降低棉球所致大鼠肉芽肿作用,二甲苯所致小鼠耳肿胀作用和二甲苯所致小鼠腹腔炎作用,与空白对照组比较,均有显著性差异(P<0.05)。三.SEA的抗炎机制研究SEA的高剂量(600mg·kg-1),中剂量(300mg·kg-1)连续三天给药,可显著降低醋酸所致小鼠腹腔炎症洗出液中PGE2和蛋清所致足肿胀小鼠炎足浸出液中MDA的量、提高小鼠眼眶血清中SOD、CAT的含量。结果表明SEA显著抑制PGE2的产生、减少MDA生成、提高SOD活性和CAT活力。结果:1.急性毒性试验表明SEA急性毒性较小,临床用药安全。2.本研究以穿心莲新制剂SEA为研究对象,主要研究了其的解热、抗炎作用,并与市售穿心莲制剂比较。与空白对照组比均有显著性差异(P<0.05),表明SEA具有显著解热、抗炎作用,且药理效应与等剂量的穿心莲制剂相当。3. SEA在抑制炎症反应的同时,可显著抑制PGE2的产生、减少MDA生成、提高SOD、CAT活性。结果提示,SEA抗炎机制可能与抑制PGE2的产生、MDA生成,提高SOD、CAT活性有关。更多还原

【Abstract】 Andrographis paniculata(Burm.f.)Nees. is a traditional Chinese drug,Supramolecular extract of Andrographis paniculata (Burm.f.) Nees. (SEA) is a new preparation which developed by Natural Drug Institute of Henan University recently. The Andrographis Paniculta is one kind of herbal drug for relieving the internal heat of the body, it has the effect of ant febrile, detoxifies,cooling blood and detumescence, so it is used to treat the heat-syndrome of the interior in the differential diagnosis.,in the medicinal works“the herbalism of Quanzhou”, there was the records for this medinical plant that it may lower febrile, detoxify, diminish inflammation and tumefaction, may be used to the throat inflammation, desentery and high fever. The previous pharmacological research indicated that the Andrographis Paniculta preparation have strong action in antipyretic, antiphlogistic, anti-bacterial and anti-viral. therefore it is widely used in clinical applies: it is applied to the fever of cold, acute and chronic pharyngitis, dysentery, ndotoxemia and so on.Objective:In this research we designed the acute toxicity and the main pharmacodynamics research of SEA preparation , and its anti-inflammation mechanism in order to offer pharmacological and experiments basis for its safe and effective use in clinic.Methods:There are three parts in this thesis:PartⅠAcute toxicity research on SEAWe observed from the pre-experiment of acute toxicity research on SEA that median lethal doses (LD50)of SEA is 717.8mg·kg-1.partⅡMain pharmacodynamics research on SEA1.Antipyretic experiments The dose of 600mg·kg -1and 300mg·kg-1 of SEA,keep on three days,can be significantly decreased high temperature induced by dried yeast in rat or 2, 4-dinitrophenol and compared to the model control group have significantly difference (p <0.01 and p <0.05).2. Anti-inflammatory experimentsThe dose of 600mg·kg-1 and 300mg·kg-1 of SEA,keep on three days ,can be significantly decreased ear edema induced by dimethylbenzene in mice, effect on granuloma hyperplasia in rat, effect on paw swell induced by egg white in rat and mouse peritoneal inflammation induced by Acetic acid. compared to the model control group have significantly difference(p <0.05).PartⅢAnti-inflammation mechanism research on SEAThe dose 600mg·kg-1 and 300mg·kg -1of SEA for three consecutive days administration can be significantly inhibited contents of PGE2 and MDA,enhance the activity of SOD and CAT.Results:1. Acute toxicity tests showed that SEA have smaller acute toxicity, it is safe for clinical use.2. In this study,we choose SEA as the new study, A major study on its anti -inflammatory and antipyretic effects, and compared with the market Chuanxinlian agents. The results showed that SEA have a significant anti-inflammatory and antipyretic effects, and have the same pharmacological effects to the same dose of Andrographolide agents.3. SEA inhibiting inflammation at the same time,could significantly inhibit the formation of PGE2、reduce the generation of MDA, enhance the activity of SOD and CAT. Results suggest that, anti-inflammatory mechanisms of SEA may related to inhibiting the formation of PGE2、reducing the generation of MDA, enhancing the activity of SOD and CAT.更多还原